Enantiospecific antitrypanosomal in vitro activity of eflornithine.

The polyamine synthesis inhibitor eflornithine is a recommended treatment for the neglected tropical disease Gambian human African trypanosomiasis in late stage. This parasitic disease, transmitted by the tsetse fly, is lethal unless treated. Eflornithine is administered by repeated intravenous infu...

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Autores principales:	Mikael Boberg, Monica Cal, Marcel Kaiser, Rasmus Jansson-Löfmark, Pascal Mäser, Michael Ashton
Formato:	article
Lenguaje:	EN
Publicado:	Public Library of Science (PLoS) 2021
Materias:	Arctic medicine. Tropical medicine RC955-962 Public aspects of medicine RA1-1270
Acceso en línea:	https://doaj.org/article/c09d0c37b3f74d8f93472961fd18e82d
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spelling	oai:doaj.org-article:c09d0c37b3f74d8f93472961fd18e82d2021-12-02T20:23:47ZEnantiospecific antitrypanosomal in vitro activity of eflornithine.1935-27271935-273510.1371/journal.pntd.0009583https://doaj.org/article/c09d0c37b3f74d8f93472961fd18e82d2021-07-01T00:00:00Zhttps://doi.org/10.1371/journal.pntd.0009583https://doaj.org/toc/1935-2727https://doaj.org/toc/1935-2735The polyamine synthesis inhibitor eflornithine is a recommended treatment for the neglected tropical disease Gambian human African trypanosomiasis in late stage. This parasitic disease, transmitted by the tsetse fly, is lethal unless treated. Eflornithine is administered by repeated intravenous infusions as a racemic mixture of L-eflornithine and D-eflornithine. The study compared the in vitro antitrypanosomal activity of the two enantiomers with the racemic mixture against three Trypanosoma brucei gambiense strains. Antitrypanosomal in vitro activity at varying drug concentrations was analysed by non-linear mixed effects modelling. For all three strains, L-eflornithine was more potent than D-eflornithine. Estimated 50% inhibitory concentrations of the three strains combined were 9.1 μM (95% confidence interval [8.1; 10]), 5.5 μM [4.5; 6.6], and 50 μM [42; 57] for racemic eflornithine, L-eflornithine and D-eflornithine, respectively. The higher in vitro potency of L-eflornithine warrants further studies to assess its potential for improving the treatment of late-stage Gambian human African trypanosomiasis.Mikael BobergMonica CalMarcel KaiserRasmus Jansson-LöfmarkPascal MäserMichael AshtonPublic Library of Science (PLoS)articleArctic medicine. Tropical medicineRC955-962Public aspects of medicineRA1-1270ENPLoS Neglected Tropical Diseases, Vol 15, Iss 7, p e0009583 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	Arctic medicine. Tropical medicine RC955-962 Public aspects of medicine RA1-1270
spellingShingle	Arctic medicine. Tropical medicine RC955-962 Public aspects of medicine RA1-1270 Mikael Boberg Monica Cal Marcel Kaiser Rasmus Jansson-Löfmark Pascal Mäser Michael Ashton Enantiospecific antitrypanosomal in vitro activity of eflornithine.
description	The polyamine synthesis inhibitor eflornithine is a recommended treatment for the neglected tropical disease Gambian human African trypanosomiasis in late stage. This parasitic disease, transmitted by the tsetse fly, is lethal unless treated. Eflornithine is administered by repeated intravenous infusions as a racemic mixture of L-eflornithine and D-eflornithine. The study compared the in vitro antitrypanosomal activity of the two enantiomers with the racemic mixture against three Trypanosoma brucei gambiense strains. Antitrypanosomal in vitro activity at varying drug concentrations was analysed by non-linear mixed effects modelling. For all three strains, L-eflornithine was more potent than D-eflornithine. Estimated 50% inhibitory concentrations of the three strains combined were 9.1 μM (95% confidence interval [8.1; 10]), 5.5 μM [4.5; 6.6], and 50 μM [42; 57] for racemic eflornithine, L-eflornithine and D-eflornithine, respectively. The higher in vitro potency of L-eflornithine warrants further studies to assess its potential for improving the treatment of late-stage Gambian human African trypanosomiasis.
format	article
author	Mikael Boberg Monica Cal Marcel Kaiser Rasmus Jansson-Löfmark Pascal Mäser Michael Ashton
author_facet	Mikael Boberg Monica Cal Marcel Kaiser Rasmus Jansson-Löfmark Pascal Mäser Michael Ashton
author_sort	Mikael Boberg
title	Enantiospecific antitrypanosomal in vitro activity of eflornithine.
title_short	Enantiospecific antitrypanosomal in vitro activity of eflornithine.
title_full	Enantiospecific antitrypanosomal in vitro activity of eflornithine.
title_fullStr	Enantiospecific antitrypanosomal in vitro activity of eflornithine.
title_full_unstemmed	Enantiospecific antitrypanosomal in vitro activity of eflornithine.
title_sort	enantiospecific antitrypanosomal in vitro activity of eflornithine.
publisher	Public Library of Science (PLoS)
publishDate	2021
url	https://doaj.org/article/c09d0c37b3f74d8f93472961fd18e82d
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Enantiospecific antitrypanosomal in vitro activity of eflornithine.

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